Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/18)
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Patent number: 5955470Abstract: This invention relates to novel amide derivatives of certain 2,6-methano-2H-quinolizine-type compounds, to the intermediates and processes for their preparation, to their ability to antagonize the effects of serotonin at the 5HT.sub.3 receptors, and to their end-use application in the treatment of chemotherapeutically-induced nausea and vomiting, as anti-anxiety agents, in the symptomatic treatment of pain associated with migraine, as anti-arrhythmic agents, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses of the type manifested in patients suffering from schizophrenia, and mania, in the treatment of glaucoma, for stimulating gastric motility, to combat drug abuse, to treat sleep apnea and to treat irritable bowel syndrome.Type: GrantFiled: October 29, 1998Date of Patent: September 21, 1999Assignee: Merrell Pharmaceuticals, Inc.Inventor: Maurice W. Gittos
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Patent number: 5932732Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound ?II!: ##STR1## wherein R.sup.o is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound ?I!: ##STR2## wherein the symbols are as defined above.Type: GrantFiled: October 28, 1997Date of Patent: August 3, 1999Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 5932587Abstract: The heterocyclic-fused pyridines are prepared by reaction of the corresponding heterocyclic-fused pyridine aldehydes with appropriately substituted Grignard or Wittig reagents. The heterocyclic-fused pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of dislipidaemia and arteriosclerosis.Type: GrantFiled: June 27, 1997Date of Patent: August 3, 1999Assignee: Bayer AktiengesellschaftInventors: Carsten Schmeck, Matthias Muller-Gliemann, Gunter Schmidt, Arndt Brandes, Rolf Angerbauer, Michael Logers, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher
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Patent number: 5922875Abstract: A compound represented by the general formula (I) shown below ##STR1## or a pharmaceutically acceptable salt thereof can be used as the active ingredient in a pharmaceutical preparation. The pharmaceutical preparation is desirable for its anti-ulcer activity, for therapeutic use against tumors sustained by gastrin and other bioactive polypeptides correlated therewith, for therapeutic use in treating disorders of the gastrointestinal tract, for the treatment of pathological conditions of the central nervous system linked to imbalances in the neural physiological levels of gastrin or other bioactive polypeptides correlated therewith, for use in the treatment and prevention of pathological eye conditions caused by surgical treatment of cataracts or chronic ocular inflammation, and for the prevention of diseases of other sensory organs.Type: GrantFiled: December 29, 1997Date of Patent: July 13, 1999Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Walter Peris, Lucio C. Rovati, Luigi A. Rovati
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Patent number: 5919788Abstract: The present invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R.sup.1 and R.sup.2 are each independently hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.3 and R.sup.4 are each independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)-amino, carboxyl, C.sub.1-6 alkyloxycarbonyl and C.sub.1-6 alkylcarbonyl; Alk is C.sub.1-4 alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 27, 1997Date of Patent: July 6, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Vandenberk, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
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Patent number: 5919790Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.Type: GrantFiled: October 2, 1997Date of Patent: July 6, 1999Assignees: Warner-Lambert Company, BASF AktiengesellsschaftInventors: Hamish John Allen, Kenneth Dale Brady, Bradley William Caprathe, Paul Galatsis, John Lodge Gilmore, Sheryl Jeanne Hays, Robert Vincent Talanian, Nigel Walker, Joseph Scott Warmus
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Patent number: 5902814Abstract: There are provided new compounds of formula I: ##STR1## wherein R represents hydrogen or methyl; andn represents 1 or 2;or a pharmaceutically acceptable acid addition salt thereof, together with processes for preparing them, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful in the treatment of psychotic disorders, intellectual impairment disorders and anxiety.Type: GrantFiled: September 18, 1995Date of Patent: May 11, 1999Assignee: Astra ABInventors: John Charles Gordon, Ronald Conrad Griffith, Robert John Murray, Michael Balestra
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Patent number: 5869496Abstract: Disclosed are spiro-substituted azacycles of formula (I), are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, emesis and asthma. In particular compounds of formula (I) are shown to be neurokinin antagonists.Type: GrantFiled: July 11, 1995Date of Patent: February 9, 1999Assignee: Merck & Co., Inc.Inventors: Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Hongbo Qi, Shrenik K. Shah
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Patent number: 5861409Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.Type: GrantFiled: April 8, 1997Date of Patent: January 19, 1999Assignee: Eli Lilly and CompanyInventors: James E. Audia, Stephen Richard Baker, Jesus Ezquerra Carrera, Carlos Lamas Peteira, Concepcion Pedregal Tercero
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Patent number: 5807865Abstract: The present invention relates to compounds of the formula (I) ##STR1## wherein X, Z, R, R.sup.1, R.sup.2, Ar, n and m are as defined herein which are of use in the treatment or prevention of neuropathy, asthma, osteoarthritis, rheumatoid arthritis or migraine.Type: GrantFiled: October 18, 1996Date of Patent: September 15, 1998Assignee: Merck Sharp & Dohme LimitedInventors: Timothy Harrison, Christopher John Swain
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Patent number: 5808071Abstract: A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of a suitable Lewis acid, and a compound capable of in situ generation of formaldehyde. The process is further characterized by formaldehyde being generated by the reaction of the Lewis acid upon the formaldehyde generating agent, instead of being present as an initial reactant. The process further avoids the presence of initial water which destroys the Lewis acid before it can act upon the formaldehyde generating agent.Type: GrantFiled: July 15, 1997Date of Patent: September 15, 1998Assignee: Hoechst Marion Roussell, Inc.Inventor: Timothy James-Norman Watson
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Patent number: 5786481Abstract: 3,7-Diazabicyclo?3.3!nonanes and selected derivatives thereof of the general formula: ##STR1## wherein Q=S; Z=CH.sub.2 ; and Y equals an N-acyl or N-alkyl group are disclosed as multiclass antiarrhythmic agents.Type: GrantFiled: October 19, 1995Date of Patent: July 28, 1998Assignee: The Board of Regents, Oklahoma State UniversityInventors: Kenneth Darrell Berlin, Gregory Lynn Garrison, Subbiah Sangiah, Cyril Roy Clarke, Chun-Lin Chen, Ralph Lazzara, Benjamin Jacob Scherlag, Eugene Stuart Patterson, George Edward Burrows
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Patent number: 5756743Abstract: Novel spiro?cyclopent?b!indole-piperidines!, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro?cyclopent?b!indole-piperidines! and intermediates, or compositions thereof are disclosed.Type: GrantFiled: February 18, 1997Date of Patent: May 26, 1998Assignee: Hoechst Marion Roussel Inc.Inventors: Mark G. Palermo, Gerard J. O'Malley
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Patent number: 5750533Abstract: There are disclosed 14.alpha.-hydroxymarcfortine derivatives of the natural products marcfortine A, B, C, and D useful in the treatment and prevention of helminth and arthropod infections of animals and plants. The synthetic derivatives are of Formula (I).Type: GrantFiled: December 7, 1995Date of Patent: May 12, 1998Assignee: Pharmacia & Upjohn CompanyInventor: Byung H. Lee
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Patent number: 5731441Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.Type: GrantFiled: October 29, 1996Date of Patent: March 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 5723616Abstract: The present invention is directed to a novel process for the preparation of the compound N-?1(R)-?(1,2-dihydro-1-methanesulfonyl-spiro?3H-indole-3,4'-piperdin!-1'- yl)carbonyl!-2-(phenylmethyl-oxy)ethyl!-2-amino-2-methyl-propanamide, and salts thereof, which has the structure: ##STR1## and which has the ability to stimulate the release of natural or endogenous growth hormone. This compound may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.Type: GrantFiled: October 23, 1996Date of Patent: March 3, 1998Assignee: Merck & Co., Inc.Inventors: Peter G. Houghton, Audrey Molina, Joannis Houpis, Joseph E. Lynch, Ralph P. Volante
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Patent number: 5684012Abstract: This subject invention relates to dimeric 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having general formula (I), ##STR1## wherein n is 1-5; R.sup.1 to R.sup.4 are substituents; R.sup.5 and R.sup.6 each hydrogen or alkyl or form together an ethylene or propylene bridge; X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, being 0 or 1, X is NR.sup.7, R.sup.7 being H, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are selected from hydroxy and the substituents defined under R.sup.7 ; and (i) Z.sup.1 is a substituent and Z.sup.2 is (CH.sub.2).sub.p wherein p is 0; and Y is N, C or CH; (ii) Z.sup.1 and Y are linked together via a single bond, thereby forming a spirocyclic junction; in which case Y is C; Z.sup.1 is O, S, (CH.sub.2).sub.q, q being 1, 2 or 3, or Z.sup.1 is CH.sub.2 O, CH.sub.2 S, CH.sub.2 CH.sub.2 O, CH.sub.2 CH.sub.2 S, CH.dbd.CH, CH.dbd.CHCH.sub.Type: GrantFiled: June 7, 1995Date of Patent: November 4, 1997Assignee: H. Lundbeck A/SInventors: Jens Perregaard, John W. Stenberg, Ejner K. Moltzen
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Patent number: 5654314Abstract: The new compounds of formulaA--O--CO--Z (I)(wherein A and Z are defined as explained in the specification) can be prepared by conventional methods; they are suitable as active substances for pharmaceutical compositions.Type: GrantFiled: March 28, 1995Date of Patent: August 5, 1997Assignee: Boehringer Ingelheim KGInventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
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Patent number: 5637709Abstract: Polychromatic compounds of pyrans having a substituted adamantane or a polycyclic ring system, with the exception of adamantane, in the 2-position of the pyran ring, having the structure ##STR1## whereby the residues R.sub.1 -R.sub.4 are independently substituents selected from the series H, alkyl, substituted phenyl, phenyl, naphthyl, OH, alkoxy (C.sub.1 -C.sub.4), halogen, alkylamino, dialkylamino, cyan, trifluormethyl, or, R.sub.1 and R.sub.2 or R.sub.3 and R.sub.4 or R.sub.2 and R.sub.3 are constituents of at least one condensed aromatic, heteroaromatic or an alkane ring, wherein said heteroaromatic ring is selected from the group consisting of pyridine, pyrimidine, pyridazine, quinoline, isoquinoline, naphthyridine, quinazoline, quinoxaline, phthalazine, pteridine, phenazine, and benzoquinoline which are substituted by the same residues as R.sub.1 -R.sub.Type: GrantFiled: February 9, 1995Date of Patent: June 10, 1997Assignee: Optische Werke G. RodenstockInventor: Manfred Melzig
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Patent number: 5635511Abstract: The use of 3,7,9,9-tetrasubstituted 3-phenylsulfonyl-3,7-diazabicyclo[3.3.1]nonane compounds for treating cardiac arrhytmias in larger mammals, including humans; novel antiarrhythmically active 3,7,9,9-tetrasubstituted compounds corresponding to the general formula Ia ##STR1## in which R.sup.1 is an alkyl group having 1-6 carbon atoms or a cycloalkylalkyl group having 4-7 carbon atoms,R.sup.2 is lower alkyl, andR.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain having 3-6 carbon atoms,R.sup.4' is cyano, an R.sup.6 --O--CO-- group in which R.sup.6 is lower alkyl, an R.sup.7 --SO.sub.2 --NH-- group in which R.sup.7 is lower alkyl, or an R.sup.8 --CO--NH-- group in which R.sup.8 is lower alkyl or a phenyl group which is optionally substituted by halogen, cyano, nitro, or an R.sup.9 --SO.sub.2 -- radical in which R.sup.9 is lower alkyl, or an imidazolyl radical located in position 4 of the phenyl ring, andR.sup.Type: GrantFiled: January 31, 1996Date of Patent: June 3, 1997Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Arman Farjam, Reinhard Brueckner, Dieter Ziegler
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Patent number: 5633248Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.Type: GrantFiled: November 21, 1995Date of Patent: May 27, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
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Patent number: 5629317Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.Type: GrantFiled: May 19, 1995Date of Patent: May 13, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Stephen R. Baker, Jesus E. Carrera, Carlos L. Peteira, Concepcion P. Tercero
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Patent number: 5610163Abstract: Compounds of the formula ##STR1## of which, in exemplary compounds, the thienyl group is attached via the 2-position and:(a) A is 3.alpha.-(6.beta., 7.beta.-epoxy)-tropanyl methobromide and R.sub.1 is 2-thienyl;(b) A is 3.alpha.-(6, 7dehydro)-tropanyl methobromide and R.sub.1 is 2-thienyl;(c) A is 3.beta.-tropanyl methobromide and R.sub.1 is 2-thienyl; and,(d) A is 3.alpha.-(N-isopropyl)-nortropanyl methobromide and R.sub.1 is cyclopentyl.These are anticholinergics. Administered by inhalation, they are useful for the treatment of chronic obstructive bronchitis or slight to moderately severe asthma. Administered by the intravenous or oral routes, they are useful for the treatment of vagally induced sinus bradycardia.Type: GrantFiled: March 16, 1995Date of Patent: March 11, 1997Assignee: Boehringer Ingelheim GmbHInventors: Rolf Banholzer, Rudolf Bauer, Richard Reichl
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Patent number: 5578593Abstract: There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: November 3, 1993Date of Patent: November 26, 1996Assignee: Merck & Co., Inc.Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
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Patent number: 5571918Abstract: A method for producing 2-methylspiro(1,3-oxathiolane-5,3')quinuclidine, which comprises reacting 3-hydroxy-3-mercaptomethylquinuclidine or a salt thereof and a carbonyl compound in the presence of a catalyst made of at least one member selected from the group consisting of tin halides, oxyacids of phosphorus, phosphorus oxyhalides and organic sulfonic acids, to produce cis-form 2-methylspiro(1,3-oxathiolane-5,3')quinuclidine or a salt thereof.Type: GrantFiled: May 11, 1995Date of Patent: November 5, 1996Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Koji Hayashi, Sho Tokumoto, Hiroshi Yoshizawa, Tatsuo Isogai, Masaru Kimura, Masahiko Sawaki, Takayoshi Ando, Isamu Katsuyama, Hayato Ariyoshi, Tadashi Nakamura
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Patent number: 5567624Abstract: A composition for determining pH of a solution comprises a fluorescent carbazine dye covalently bound to a solid support. A method of determining pH of a solution comprises placing the composition in the solution, contacting the composition with a selected wavelength of light to excite fluorescence by the carbazine dye, measuring intensities of the fluorescence at two selected wavelengths, calculating a ratio of fluorescence intensities at the two selected wavelengths, and correlating the ratio with a predetermined relationship of such ratios to pH. A fiber optic system for measuring pH of a solution with the carbazine-dye-containing composition is also disclosed.Type: GrantFiled: April 27, 1995Date of Patent: October 22, 1996Assignee: Utah Medical Products, Inc.Inventor: Roger E. Smith
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Patent number: 5554620Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.Type: GrantFiled: July 29, 1994Date of Patent: September 10, 1996Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5547958Abstract: 8.alpha.-acylamino ergolines are useful dopamine agonists.Type: GrantFiled: December 27, 1994Date of Patent: August 20, 1996Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter-Andreas Loschmann
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Patent number: 5545834Abstract: Methods are disclosed for determining an analyte in a medium suspected of containing the analyte. One method comprises providing (1) combining a medium suspected of containing the analyte and a novel chemiluminescent compound, (2) combining a means for chemically activating the chemiluminescent compound; and (3) detecting the amount of luminescence generated by the chemiluminescent compound. The amount of luminescence generated is related to the amount of analyte in the medium. The chemiluminescent compound can be chemically activated by hydrogen peroxide. Compositions and kits are also disclosed.Type: GrantFiled: January 17, 1995Date of Patent: August 13, 1996Assignee: Behringwerke AGInventors: Sharat Singh, Rajendra Singh, Frank Meneghini, Edwin F. Ullman
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Patent number: 5536716Abstract: There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: November 3, 1993Date of Patent: July 16, 1996Assignee: Merck & Co., Inc.Inventors: Meng-Hsin Chen, David B. R. Johnston, Ravi P. Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang
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Patent number: 5532255Abstract: Compounds of the formula ##STR1## in which R.sup.1, X and Y have the meanings defined herein, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and tumors.Type: GrantFiled: April 29, 1994Date of Patent: July 2, 1996Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Peter Raddatz, Joachim Gante, Horst Juraczyk, Hanns Wurziger, Helmut Prucher, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5532361Abstract: Photochromic compounds belonging to the class of spiro-pyrans, having the general formula (I): ##STR1##Type: GrantFiled: May 12, 1994Date of Patent: July 2, 1996Assignee: Ministero Dell `Universita` E Della Ricerca Scientifica E TechnologicaInventors: Pietro Allegrini, Nereo Nodari, Vincenzo Malatesta, Luciana Crisci
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Patent number: 5527912Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino) alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.Type: GrantFiled: March 27, 1995Date of Patent: June 18, 1996Assignee: Pfizer Inc.Inventor: Bertrand L. Chenard
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Patent number: 5498614Abstract: The invention relates to bridged aza-bicyclic derivatives of formula (I). These compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. Also disclosed are intermediates used in the synthesis of compound of formula (I).Type: GrantFiled: November 7, 1994Date of Patent: March 12, 1996Assignee: Pfizer Inc.Inventor: Manoj C. Desai
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Patent number: 5493029Abstract: The present invention relates to novel benzopyran derivatives of formula (I) which have exellent effectiveness in the treatment of asthma as well as hypertension. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, F, Cl or H, except for that X.sub.1, X.sub.2 and X.sub.3 may not be hydrogen atom simulaneously; R.sup.A and R.sup.B are, each independently, a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group; and R.sup.C and R.sup.D are, each independently, a hydrogen atom or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is a C.sub.1-4 straight or branched alkyl group;R.sub.3 is a C.sub.Type: GrantFiled: December 9, 1993Date of Patent: February 20, 1996Assignee: Korea Research Institute of Chemical TechnologyInventors: Sung-Eun Yoo, Kyu Y. Yi, Nak C. Jeong, Jee H. Suh, Seon-Ju Kim, Hwa-Sup Shin, Byung H. Lee, Kyu S. Jung
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Patent number: 5484923Abstract: The present invention is directed to a process of making spirocycles of general structural formula: ##STR1## where R.sub.1 is selected from the group consisting of CO--C.sub.1-3 alkyl, cyano, carboxy, carboxy C.sub.1-6 alkyl ester, carboxamide, C.sub.1-6 alkyl sulfinyl, C.sub.1-6 alkyl sulfonyl, C.sub.1-6 methanesulfonamide and halogen; R.sub.2 is selected from the group consisting of keto or alcohol, R.sub.3 is cyano, resulting in compounds which are Class III antiarrhythmic.Type: GrantFiled: May 31, 1994Date of Patent: January 16, 1996Assignee: Merck & Co., Inc.Inventors: Dongwei Cai, Richard Desmond, Yao-Jun Shi, David M. Tschaen, Thomas R. Verhoeven
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Patent number: 5472968Abstract: Compounds of formula (I), ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen, C.sub.1-6 alkyl, R.sub.3 and R.sub.4 independently represent one or more radicals selected from hydrogen, OH, NH.sub.2, NO.sub.2, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy and n is an integer from 1-2 inclusive, and pharmaceutically acceptable derivatives thereof are useful as pharmaceuticals; in particular, they possess N-methyl-(d)-aspartate(NMDA) blocking properties and are useful in the treatment and/or prevention of neurodegenerative conditions.Type: GrantFiled: March 16, 1993Date of Patent: December 5, 1995Assignee: Fisons CorporationInventors: Ronald C. Griffith, James R. Matz, James J. Napier
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Patent number: 5468858Abstract: 3,7-Diazabicyclo[3.3.1]nonanes and selected derivatives thereof of the general formula: ##STR1## are disclosed as multiclass antiarrhythmic agents.Type: GrantFiled: October 28, 1993Date of Patent: November 21, 1995Assignee: The Board of Regents of Oklahoma State University Physical SciencesInventors: Kenneth D. Berlin, Gregory L. Garrison, Subbiah Sangiah, Cyril R. Clarke, Chun-Lin Chen, Ralph Lazzara, Benjamin J. Scherlag, Eugene S. Patterson, George E. Burrows
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Patent number: 5414088Abstract: The invention concerns compounds of formula I ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl, R.sup.2 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, cyano, carboxy [carbonyl substituted by hydroxyl], C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino or hydrazino or R.sup.1 and R.sup.2 together are C.sub.2 -C.sub.6 -alkylidene or C.sub.3 -C.sub.6 -cycloalkylidene or R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, form a C.sub.3 -C.sub.7 -spirocycle, n is 0 or 1, R.sup.3 is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.7 -cycloalkyl, benzyl, carboxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkyloxycarbonyl-C.sub.1 -C.sub.6 -alkyl or di-C.sub.1 -C.sub.6 -alkyloxophosphinyl-C.sub.1 -C.sub.6 -alkyl and R.sup.4 -R.sup. 6 are as in the specification.Type: GrantFiled: April 14, 1992Date of Patent: May 9, 1995Assignee: Boehringer Mannheim GmbHInventors: Wolfgang Von Der Saal, Harald Zilch, Erwin Bohm
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Patent number: 5391748Abstract: The present invention relates to dihydroquinolines of formula (I): ##STR1## in which the symbols used are as defined in the description, to a process for their preparation, to their use in recording materials and to recording materials in which such dihydroquinolines are present.Type: GrantFiled: December 3, 1993Date of Patent: February 21, 1995Assignee: Bayer AktiengesellschaftInventor: Horst Berneth
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Patent number: 5391742Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.Type: GrantFiled: April 15, 1994Date of Patent: February 21, 1995Assignee: Pfizer Inc.Inventor: Bertrand L. Chenard
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Patent number: 5369084Abstract: Isonicotinic acid derivatives and related furo-, thieno- and pyrrolo[3,4-c]pyridin-1(3H)-one, -thione and -imine compounds having the formula ##STR1## wherein R is ##STR2## Q is O, S or NR.sup.7 ; Y is O, S or NR.sup.8 ; L is COOR.sup.9, CONR.sup.10 R.sup.11, C(.dbd.S)NR.sup.10 R.sup.11, CN, or a radical of formula ##STR3## the acceptable addition salts, the stereochemically isomeric forms and the N-oxides thereof, having herbicidal properties, compositions containing the same and methods for controlling weeds.Type: GrantFiled: May 6, 1993Date of Patent: November 29, 1994Assignee: Janssen Pharmaceutical N.V.Inventors: Hans-Rudolf Waespe, Guy R. E. Van Lommen, Victor K. Sipido
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Patent number: 5332746Abstract: The invention relates to a group of new 8,9-annelated-.beta.-carbolines and 8,9-annelated-3,4-dihydro-.beta.-carbolines having interesting fibrinolytic properties. In particular the compounds can be used as orally active fibrinolytics.The compounds have the general formulae 1 and 2 ##STR1## wherein R.sub.2 +R.sub.3 together with the carbon atom and the nitrogen atom to which they are bound and the intermediate carbon atom constitute a heterocyclic group consisting of 5-10 ring atoms.Type: GrantFiled: May 8, 1991Date of Patent: July 26, 1994Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Hans H. Haeck, Ineke van Wijngaarden, Johannes W. C. M. Jansen
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Patent number: 5324732Abstract: 1.5 Fumaric acid salts of N,N'-di-lower alkyl-substituted 9,9-alkylene-3,7-diazabicyclo[3.3.1 ]nonanes and a process for obtaining them in stoichiometrically pure and virtually non-hygroscopic form.Type: GrantFiled: November 23, 1992Date of Patent: June 28, 1994Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Walter Heitmann, Uwe Maetzel
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Patent number: 5300511Abstract: The present invention relates to novel benzopyran derivatives of formula(I) which have exellent effectiveness in the treatment of asthma as well as hypertension. ##STR1## wherein R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, F, Cl or H, except for that X.sub.1, X.sub.2 and X.sub.3 may not be hydrogen atom simulaneously; R.sup.A and R.sup.B are, each independently, a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group; and R.sup.C and R.sup.D are, each independently, a hydrogen atom or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is a C.sub.1-4 straight or branched alkyl group;R.sub.3 is a C.sub.Type: GrantFiled: May 21, 1992Date of Patent: April 5, 1994Assignee: Korea Research Institute of Chemical TechnologyInventors: Sung-Eun Yoo, Kyu Y. Yi, Nak C. Jeong, Jee H. Suh, Seon-Ju Kim, Hwa-Sup Shin, Byung H. Lee, Kyu S. Jung
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Patent number: 5292747Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, m, n, p, and q are as set forth in the specification, as well as pharmaceutically acceptable salts of acidic compounds of formula I with bases and of basic compounds of formula I with acids, which are useful in the control or prevention of inflammatory, immunological, oncological, bronchopulmonary, dermatological or cardiovascular disorders or for the treatment of asthma, AIDS or diabetic complications or for the stimulation of hair growth are described.Type: GrantFiled: September 21, 1992Date of Patent: March 8, 1994Assignee: Hoffman-La Roche Inc.Inventors: Peter D. Davis, Christopher H. Hill, Goeffrey Lawton
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Patent number: 5292746Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.Type: GrantFiled: August 5, 1992Date of Patent: March 8, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, Craig E. Thomas, Ronald C. Bernotas, George Ku
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Patent number: 5281710Abstract: A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.Type: GrantFiled: September 1, 1992Date of Patent: January 25, 1994Assignee: The Scripps Research InstituteInventors: Adrian L. Smith, Chan-Kou Hwang, Sebastian V. Wenderborn, Kyriacos C. Nicolaou, Erwin P. Schreiner, Wilhelm Stahl, Wei-Min Dai, Peter E. Maligres, Toshio Suzuki
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Patent number: 5254564Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, .sup.4 or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group;R.sub.4 and R.sub.5 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group; R.sub.6 and R.sub.7 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group;or R.sub.5 and R.sub.6 are together --CH.sub.2 -- when each of R.sub.4 and R.sub.7 is hydrogen or C.Type: GrantFiled: July 16, 1990Date of Patent: October 19, 1993Assignee: Lo Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Giuseppe Giardina, Roberto Colle
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Patent number: 5227488Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; X represents oxygen or sulfur; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.Type: GrantFiled: September 28, 1990Date of Patent: July 13, 1993Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Peter H. Andersen, Louis B. Hansen, Peter Faarup, John B. Hansen